2-PyriMidinaMine, 4-(4-fluoro-1-naphthalenyl)-6-(1-Methylethyl)-, Monohydrochloride
- Product Name
- 2-PyriMidinaMine, 4-(4-fluoro-1-naphthalenyl)-6-(1-Methylethyl)-, Monohydrochloride
- CAS No.
- 199864-86-3
- Chemical Name
- 2-PyriMidinaMine, 4-(4-fluoro-1-naphthalenyl)-6-(1-Methylethyl)-, Monohydrochloride
- Synonyms
- MT 500 Hydrochloride;RS 127445 hydrochloride NEW;RS-127445 hydrochloride, 10 mM in DMSO;4-(4-Fluoro-1-naphthyl)-6-isopropylpyriMidin-2-aMine;2-Amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine hydrochloride;2-AMino-4-(4-fluoronaphth-1-yl)-6-isopropylpyriMidine Monohydrochloride;4-(4-Fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinamine monohydrochloride;2-PyriMidinaMine, 4-(4-fluoro-1-naphthalenyl)-6-(1-Methylethyl)-, Monohydrochloride
- CBNumber
- CB42609717
- Molecular Formula
- C17H17ClFN3
- Formula Weight
- 317.7883832
- MOL File
- 199864-86-3.mol
2-PyriMidinaMine, 4-(4-fluoro-1-naphthalenyl)-6-(1-Methylethyl)-, Monohydrochloride Property
- Melting point:
- 158 °C
- storage temp.
- 2-8°C
- solubility
- DMSO: ≥20mg/mL
- form
- powder
- color
- white to tan
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H301Toxic if swalloed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- R2533
- Product name
- RS-127445 hydrochloride
- Purity
- ≥98% (HPLC), powder
- Packaging
- 5mg
- Price
- $133
- Updated
- 2025/07/31
- Product number
- R2533
- Product name
- RS-127445 hydrochloride
- Purity
- ≥98% (HPLC), powder
- Packaging
- 25mg
- Price
- $514
- Updated
- 2025/07/31
- Product number
- R0221
- Product name
- RS-127445 Hydrochloride
- Packaging
- 10MG
- Price
- $190
- Updated
- 2025/07/31
- Product number
- R0221
- Product name
- RS-127445 Hydrochloride
- Packaging
- 50MG
- Price
- $680
- Updated
- 2025/07/31
- Product number
- 23451
- Product name
- RS 127445 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 1 mg
- Price
- $32
- Updated
- 2024/03/01
2-PyriMidinaMine, 4-(4-fluoro-1-naphthalenyl)-6-(1-Methylethyl)-, Monohydrochloride Chemical Properties,Usage,Production
Uses
RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi=9.5) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
Biological Activity
RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi=9.5) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
in vivo
In rats, the fraction of RS-127445 that is bioavailable via the oral or intraperitoneal routes is 14 and 60% respectively. Intraperitoneal administration of RS-127445 (5 mg/kg) produced plasma concentrations predicted to fully saturate accessible 5-HT2B receptors for at least 4 h.RS-127445 (5 mg/kg) is administered to rats by oral, intraperitoneal and intravenous routes. Peak plasma concentrations are rapidly achieved with the highest concentrations being found at the first time-point measured following intravenous and intraperitonael administration (0.08 h) and by 0.25 h following dosing by the oral route of administration. RS-127445 is cleared from plasma with an estimated terminal elimination half-life of approximately 1.7 h. The bioavailability of RS-127445, when administered by the oral and intraperitoneal routes is approximately 14 and 62% of that obtained by intravenous administration. Approximately 60% of an intraperitoneal dose and 14% of the oral dose of RS-127445 (5 mg/kg) is bioavailable[1]. RS-127445 (1-30 mg/kg), dose-dependently reduces faecal output, reaching significance at 10 and 30 mg/kg (n=6-11). In blood and brain, >98% of RS-127445 is protein-bound[2].
IC 50
sPLA2: 5.5 (pKi); 5-HT3 Receptor: <6 (pKi); 5-HT5 Receptor: <6 (pKi); 5-HT6 Receptor: <6 (pKi); 5-HT2A Receptor: 6.3 (pKi); 5-HT2C Receptor: 6.4 (pKi); 5-HT2B Receptor: 9.5 (pKi)
storage
Desiccate at +4°C
2-PyriMidinaMine, 4-(4-fluoro-1-naphthalenyl)-6-(1-Methylethyl)-, Monohydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
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